Sigma-Tau Industrie Farmaceutiche Riunite S.p.a.

Istituto Nazionale Per Lo Studio E La Cura Dei Tumori

Other

Sigma-Tau

Instituto Nazionale Per Lo Studio E La Cura Dei Tumori

Sigma-Tau Healthscience S.p.a.

Sigma-Tau Farmaceutiche Riunite, S.p.a.

501 Sigma Tau Industrie Farmaceutiche Riunite S.p.a.

Maria Ornella Tinti

Mauro Marzi

Fabio Giannessi

Domenico Misiti

Francesco De Angelis

Nazareno Scafetta

Claudio Pisano

Piero Foresta

Claudio Cavazza

Patrizia Minetti

Paolo De Witt

Giuseppe Giannini

Orlando Ghirardi

Sergio Penco

Mose Santaniello

Carlo A Bagolini

Domenico Alloatti

Emma Quaresima

Paolo Carminati

Loredana Vesci

Franco Zunino

Arduino Arduini

Piero Chiodi

Walter Cabri

Marco Alpegiani

Carlo Scolastico

Lucio Merlini

Domenico Vergani

Giovanni Salvatori

Paolo DeWitt

Fabrizio Giorgi

Paolo Ghetti

Natalina Dell'Uomo

Luciana Critelli

Roberto Cozzolino

Sabrina Dallavalle

Roberto Castagnani

Vito Ulderico Ruggiero

Maria Laura Bolognesi

Emanuela Tassoni

Vesci Loredana

Zunino Franco

Alma Dal Pozzo

Mosé Santaniello

Mos&eacute; Santaniello

Pompeo Pessotto

Mos&egrave; Santaniello

Oreste Piccolo

Maurizio Botta

Fausto Bonifacio

Gian Piero Moretti

Maria Assunta Di Cesare

Teresa Riccioni

Cristina Crescenzi

Tiziana Brunetti

Carla Franceschelli

Pederico Corelli

Carlo Sclolastico

Massimo Castorina

Licia Pacifici

Romano Di Fabio

Ida Bernabei

Gian Carlo Gramiccioli

Paolo deWitt

Maria Grazia Cima

Ni Minghong

Ni Ming Hong

Marcella Marcellini

Caludio Pisano

Anna Floriana Sciarroni

Ferdinando Maria Milazzo

Elena Marastoni

Cabri Walter

Alpegiani Marco

Vergani Domenico

Danelli Tamara

Gomez Patricio Martin

Penco Sergio

Nicola Fanto′

Enrico Garattini

Andrea Pucci

Lucia Critelli

Monica Bandera

Fabio Giannesi

Ni Ming Hong Hong

Martin Gomez Patricio

A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process.

Stereoselective process and crystalline forms of a camptothecin

Described herein are both non-hygroscopic salts of L-carnitine and alkanoyl L-carnitine with taurine chloride (2-aminoethane-sulphonic chloride) and non-hygroscopic salts of L-carnitine and alkanoyl L-carnitine with glycine chloride which lend themselves favorably to the preparation of solid compositions suitable for oral administration. Also described are solid compositions containing said salts.

Solid compositions suitable for oral administration containing non-hygroscopic salts of L-carnitine and the alkanoyl L-carnitines with taurine chloride and glycine chloride

Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH&#x2014;CHC&#x2550;CH; R is hydrogen, halogen, C-Calkoxy, C-Calkylthio, C-Calkyl, C-Ccycloalkyl; Ris 1-peperazinyl, 1-homopiperazinyl and 1-piperidinyl; Ris hydrogen, C-Calkoxy, C-Calkylthio, C-Calkyl, CHO, CH&#x2550;NOH,CHOH. The formula (I) compounds are endowed with characteristic atypical anti-psychotic activity, and are therefore useful as medicaments, in particular for the treatment and prevention of schizophrenia, paranoid states, manic-depressive states, disorders of the affective sphere, social regression, personality regression, and hallucinations. Said compounds also present advantageous pharmacokinetic properties.

Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity

Compounds of Formula (I) are described in which the Rgroup is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors &#x3b1;&#x3b2;and &#x3b1;&#x3b2;and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.

Camptothecins conjugated in position 7 to cyclic peptides as cytostatic agents

Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase

Esters of L-carnitine and alkanoyl L-carnitines are described which can be used as cationic lipids for the intracellular delivery of pharmacologically active compounds. New esters of L-carnitine and alkanoyl L-carnitines of formula (I) are also disclosed wherein the R groups are as defined in the description.

Esters of L-carnitine of alkanoyl L-carnitines useful as cationic lipids for the intracellular delivery of pharmacologically active compounds

Compounds are disclosed with the general formula in which the groups are as defined in the description here below and characterized by the presence of polyamine substituents on the imine/oxime residue, such amine groups being in turn protected by suitable protective groups. Said compounds are endowed with potent topoisomerase I inhibiting activity and therefore are useful as medicaments for the treatment of tumors and viral and parasite infections.

7-Polyaminoalkyl(oxy)iminomethylcamptothecins bearing protective groups

Compounds of Formula (I) are described: in which the Rgroup is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors &#x3b1;&#x3b2;and &#x3b1;&#x3b2;and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.

7-t-butoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists

Esters of L-carnitine or alkanoyl L-carnitines useful as cationic lipids for the intracellular delivery of pharmacologically active compounds

The present invention is related to new derivatives of Combretastatin, of Formula obtained by total synthesis. The strategy developed for each of the compounds is to i) replace a halogen (i.e. fluorine atom) to hydrogen on olefinic bound; ii) replace an aromatic ring in a natural product with an amino-aromatic ring. Said compounds recognize and bind the tubulin site: are useful for treating pathological states which arise from or are exacerbated by cell proliferation&#x2014;as anticancer and/or antiangiogenic activity, in a mammal&#x2014;to pharmaceutical compositions comprising these compounds.

Fluorocombretastatin and derivatives thereof

Compounds of formula (I)wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.

Formula (I) compounds are described: (I) where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors. 

Esters in position 20 of camptothecins

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Rome, Italy

Maria Ornella Tinti